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Synthesis and biological evaluation of novel thiazolidinedione analogues as 15-hydroxyprostaglandin dehydrogenase inhibitors.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2011 Jul 28; Vol. 54 (14), pp. 5260-4. Date of Electronic Publication: 2011 Jun 29. - Publication Year :
- 2011
-
Abstract
- Novel thiazolidinedione analogues as 15-hydroxyprostaglandin dehydrogenase (15-PGDH) inhibitors were synthesized. Compounds 2, 3, and 4 exhibited IC(50) of 25, 8, and 19 nM, respectively. They also significantly increased levels of PGE(2) in A549 cells. To assess the influence of 15-PGDH inhibitor on cochlear blood flow (CBF), 2 was applied intravenously to guinea pigs. It increased their CBFs. Scratch wounds were also analyzed in confluent monolayers of HaCaT cells. Cells exposed to 4 showed significantly improved wound healing with respect to a control.
- Subjects :
- Animals
Cell Line, Tumor
Cochlea blood supply
Cochlea drug effects
Cyclooxygenase 1 biosynthesis
Cyclooxygenase 2 biosynthesis
Dinoprostone biosynthesis
Guinea Pigs
Humans
Male
Multidrug Resistance-Associated Proteins biosynthesis
Organic Anion Transporters biosynthesis
Structure-Activity Relationship
Thiazolidinediones chemistry
Thiazolidinediones pharmacology
Wound Healing drug effects
Hydroxyprostaglandin Dehydrogenases antagonists & inhibitors
Thiazolidinediones chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 1520-4804
- Volume :
- 54
- Issue :
- 14
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 21650226
- Full Text :
- https://doi.org/10.1021/jm200390u